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MMV s distinct mode of inhibition addresses key impediments
2021-12-15

MMV019313's distinct mode of inhibition addresses key impediments in the development of PfFPPS/GGPPS inhibitors as antimalarial drugs. First, it is the first non-bisphosphonate inhibitor of Plasmodium FPPS/GGPPS with drug-like physicochemical properties satisfying the “Rule of 5” (Van Voorhis et al.
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br Significance Cellular heterogeneity for
2021-12-15

Significance Cellular heterogeneity for phenotypic features is a key mechanism underlying disease progression and therapeutic resistance, yet its regulation is poorly understood at the molecular level. Our findings demonstrate that endocrine resistance is associated with higher transcriptomic het
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YAP TAZ nuclear function is also influenced
2021-12-15

YAP/TAZ nuclear function is also influenced by interaction with the TEAD family of transcription factors [96, 97, 98, 99, 100, 101]. The RAC1 blue nitro exchange factor protein TIAM1 has recently been linked to YAP/TAZ regulation in the nucleus and cytoplasm. Nuclear TIAM1 inhibits YAP/TAZ binding
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br Conclusion br Acknowledgments This research was funded by
2021-12-15

Conclusion Acknowledgments This research was funded by Tianjin Health Institution Key Projects, grant number 15KG148” and “Tianjin Medical University General Hospital Youth Incubation Fund, grant number ZYYFY2017029”. I would like to express my heartfelt gratitude to Professor Hongtao Zhang fo
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Bilirubin Further SAR was explored with the imidazole series
2021-12-15

Further SAR was explored with the imidazole series to achieve better enzyme inhibition activity (). In comparison to published earlier, replacing the amide with sulfonamide and reverse sulfonamide maintained the GSNOR inhibitory activity. It is clear that exchanging the phenyl ring (, and ) by t
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We addressed the role of GSNOR mediated T cell activation
2021-12-15

We addressed the role of GSNOR-mediated T-cell activation in HHcy-accelerated atherosclerosis in vivo by two mouse models. Generated for the first time, GSNOR-/-ApoE-/- double knock-out mice showed decreased atherosclerosis in aortic roots in response to HHcy. The specificity of GSNOR ablation in T
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br The mode of binding of ligands
2021-12-15

The mode of binding of ligands to GPR35 As noted above, although kynurenic Cilnidipine synthesis is an agonist at GPR35, this is true for neither kynurenine [8] nor kynurenic acid ethyl ester [13]. This implicates a key role for the carboxylate group in binding and/or activation of GPR35. Import
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antimalaria medication The simple carrier model for GLUT tra
2021-12-15

The simple carrier model for GLUT1 transport activity proposes that the transporter alternates between an outward facing glucose binding site and an inward, cytoplasmic, facing glucose binding site. Cytochalasin B is an endofacial inhibitor and appears to preferentially bind to the open, inward faci
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The identification of distinct expression domains
2021-12-15

The identification of distinct expression domains in the limb suggested that these domains might have specific biological functions. We explored this possibility by determining enriched biological processes for each category using GO ontology term analysis (WebGestalt) (Zhang et al., 2005). Category
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Ionotropic aminobutyric acid GABA receptors GABARs
2021-12-15

Ionotropic γ-aminobutyric WM-8014 (GABA) receptors (GABARs) belong to the Cys-loop ligand-gated ion channel (LGIC) superfamily and play an important role in the rapid inhibitory synaptic transmission in nervous systems of both vertebrate and invertebrate (Buckingham et al., 2005). Insect ionotropic
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Introduction Initially postulated to represent the main
2021-12-15

Introduction Initially postulated to represent the main source of ATP production in eukaryotic cells, mitochondria are recently recognized to perform manifold essential functions beyond energy production, impacting most areas of cell biology and medicine [1]. Mitochondrial metabolism is both the ba
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Ropinirole HCl Free fatty acids FFAs which are obtained from
2021-12-14

Free fatty acids (FFAs), which are obtained from dietary fat or endogenous synthesis, function as nutrients and signaling molecules. Studies have shown that free fatty Ropinirole HCl receptors 1–4 which are G-protein coupled receptors, bind free fatty acids and serve as receptors for these FFAs. Sh
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Neither E nor Z FPP synthase
2021-12-14

Neither E- nor Z-FPP synthase catalyzed the reaction between 8-THPOGPP and IPP. However, a mutant E-FPP synthase (Y81S) produced 12-THPOFPP from the substrates 8-THPOGPP and IPP, and wild-type E-FPP synthase catalyzed the reaction betweeen 8-AcOGPP and IPP producing 12-AcOFPP. Mutant E-FPP synthase
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The cases of the Berlin and London patients also
2021-12-14

The cases of the Berlin and London patients also highlight our limits to defining an HIV cure. No signs of the virus have been found in numerous assays with multiple samples from diverse tissues that Timothy Brown has generously contributed to advance research over the past 12 years. In the case of
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Introduction Pneumocystis pneumonia PCP is a respiratory
2021-12-14

Introduction Pneumocystis pneumonia (PCP) is a respiratory invasive infection caused by Pneumocystis jirovecii, an ubiquitous fungus. It is transmitted by air and mostly infects immunocompromised patients. PCP is characterized by respiratory complaints of cough, dyspnea, but also tachycardia, low g
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